Comparative Pharmacology
Head-to-head clinical analysis: GABLOFEN versus SOMA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GABLOFEN versus SOMA.
GABLOFEN vs SOMA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
GABLOFEN (baclofen) is a GABA-B receptor agonist that reduces spinal reflex transmission and inhibits excitatory neurotransmitter release.
Centrally acting muscle relaxant; acts at brainstem reticular formation and spinal cord levels to inhibit polysynaptic reflexes, possibly via GABAergic and monoaminergic pathways.
10 mg orally three times daily, may increase by 10 mg/day every 3 days to a maximum of 80 mg/day (20 mg four times daily).
250 mg to 350 mg orally three times daily and at bedtime.
None Documented
None Documented
Terminal half-life 5-7 hours; clinically relevant for dosing interval of every 6-8 hours.
Clinical Note
moderateSomatostatin + Cyclosporine
"The serum concentration of Cyclosporine can be decreased when it is combined with Somatostatin."
Clinical Note
moderateSomatostatin + Methylphenobarbital
"The risk or severity of adverse effects can be increased when Somatostatin is combined with Methylphenobarbital."
Clinical Note
moderateSomatostatin + Hexobarbital
"The risk or severity of adverse effects can be increased when Somatostatin is combined with Hexobarbital."
Clinical Note
moderate1-2 hours; prolonged to 3-4 hours in hepatic impairment; parent drug rapidly cleared via CYP2C19 metabolism to meprobamate (active, t1/2 6-16 hours).
Renal: 70-80% unchanged; biliary/fecal: <5% as metabolites. Total clearance 2.5-3.0 L/h.
Renal: ~60-70% as metabolites (including meprobamate and glucuronide conjugates); fecal: minimal; biliary: negligible.
Category C
Category C
Skeletal Muscle Relaxant
Skeletal Muscle Relaxant
Somatostatin + Thiamylal
"The risk or severity of adverse effects can be increased when Somatostatin is combined with Thiamylal."